Science Time Machine | Aspirin, the “magic drug” that changed the world

March 6, 1899

The birth of aspirin, the "magic drug" that changed the world

There is a medicine that you may not have taken, but you must have heard of it. This is the well-known aspirin. Since its discovery more than 120 years ago, aspirin has developed from an unknown ingredient in willow bark to a commonly used medicine trusted by the world.

Aspirin is a non-steroidal anti-inflammatory drug, and its core ingredient is acetylsalicylic acid. In 1897, German chemist Felix Hofmann first discovered the drug and officially launched it on the market on March 6, 1899. As one of the three classic drugs in the pharmaceutical field, aspirin is still the most widely used antipyretic, analgesic and anti-inflammatory drug in the world, and is also used as a benchmark preparation for measuring and comparing other similar drugs.

From willow leaves to salicylic acid

"Magic medicine" has long been around human beings

Li Shizhen, a pioneer of Chinese pharmacology, wrote in his masterpiece Compendium of Materia Medica: "Willow leaves can cure erysipelas in children. Take one pound of willow leaves, add one bucket of water and boil, and get three liters of juice. Wash the affected area seven to eight times a day." This record may be the earliest written material about the anti-inflammatory effect of willow leaves in my country. In ancient Egypt, as early as more than 2,000 years BC, there were also records about the analgesic effect of willow leaves, indicating that some components in willow leaves have anti-inflammatory and analgesic effects.

After unremitting exploration by pharmacists and chemists of later generations, the active ingredient "salicin" was finally successfully isolated from willow bark. Subsequently, through further purification, the more active salicylic acid was obtained and its artificial synthesis was achieved.

At this point, salicylic acid preparations, the predecessor of aspirin, have been used clinically. However, although the drug has shown good anti-inflammatory and analgesic effects, its side effects cannot be ignored. After taking it, some patients feel nausea and vomiting due to the unique odor of salicylic acid, and even have adverse reactions such as gastric ulcers and acidosis, and the treatment experience is poor.

Therefore, at that time, although salicylic acid preparations had begun to be used to treat rheumatism, arthritis and other diseases, their strong odor and side effects still deterred many patients.

The birth of aspirin is due to the doctor's filial piety

The father of Hoffmann, a German chemist and patent applicant for aspirin, was an arthritis patient. In order to enable his father to take safe and smooth medicine as soon as possible, he was determined to overcome the difficulty of salicylic acid.

After unremitting efforts, Hofmann's team successfully added an acetyl group to the salicylic acid molecule, and the resulting acetylsalicylic acid effectively solved the problem. The addition of the acetyl group can be said to be the finishing touch, which significantly neutralizes the irritation of salicylic acid, can effectively protect the gastric mucosa of the human body, and improves the performance of the drug.

After sufficient animal and human trials, the drug was officially patented on March 6, 1899, and the famous "Aspirin" was officially born. The name Asprin comes from the acetyl group (Acetyl) and the shrub Spireae (Spireae) from which salicylic acid is derived. Aspirin was widely praised as soon as it was launched on the market, bringing huge profits to the German Bayer company. Despite the subsequent disputes over property rights, the influence of aspirin continues to this day, and Hoffman's filial piety is also praised by future generations.

The reason why aspirin has become one of the three classic drugs in the world is not just because of its antipyretic and analgesic effects. As an evergreen in the history of medicine, aspirin benefits from its own excellent effects as well as the development of medicine and pharmacy. Scientists' continuous research continues to explore the efficacy of aspirin, making it a versatile drug in clinical use.

The Spanish Flu: A War That Became a God

Aspirin first came into the public eye during the Spanish flu pandemic in 1918.

At that time, as the epidemic spread rapidly, the sales of aspirin in pharmacies soared, becoming the first choice for people to relieve the pain, discomfort and other symptoms caused by influenza. At the same time, the influenza epidemic has escalated into a global pandemic, causing huge casualties. According to reports at the time, aspirin showed significant effects in alleviating influenza symptoms and also expanded its scope of use. Therefore, the Spanish flu unexpectedly accelerated the popularity of aspirin to a certain extent, making it one of the best-selling drugs of the period.

Entering the World War II, the role of aspirin has undergone a new transformation, playing a key role in the victory of the war. On the one hand, aspirin is widely used in the treatment of war wounds and has become an indispensable first aid drug on the battlefield. Faced with a large number of injured soldiers in urgent need of treatment, aspirin, with its excellent analgesic, cooling and anti-inflammatory effects, effectively alleviated the soldiers' pain and improved the treatment effect. On the other hand, given that soldiers are in a state of stress for a long time and have less exercise in a war environment, they are prone to thrombotic diseases. As a platelet aggregation inhibitor, aspirin plays an important role in preventing thrombosis, significantly reducing the incidence of thrombosis in soldiers and ensuring their health and combat effectiveness.

Since then, aspirin has gradually established its core position in modern medicine and has become one of the indispensable therapeutic drugs.

Aspirin becomes a deity

Aspirin, as a classic antipyretic analgesic and non-steroidal anti-inflammatory drug, was initially used to treat arthritis, colds, and flu, and has significant antipyretic, analgesic, and anti-inflammatory effects. However, the specific pharmacological mechanism of aspirin (i.e., salicylic acid preparations) was not clear in the early days.

In 1971, British scientists John Venn and Professor Priscilla Piper jointly revealed the key mechanism of aspirin's efficacy: the drug effectively relieves or eliminates fever, pain and inflammation caused by prostaglandins by inhibiting the synthesis of prostaglandins in the body. Through in-depth research, they found that aspirin's inhibitory effect on prostaglandin synthesis is mainly attributed to its inhibition of cyclooxygenase-1 (COX-1) production. COX-1 is a key enzyme that promotes platelet aggregation. Its inhibition causes aspirin to have anti-platelet aggregation and anti-thrombotic effects. Therefore, patients who have undergone heart stent surgery need to take aspirin for a long time to reduce the risk of blood vessel blockage again.

Aspirin's remarkable antithrombotic effect makes it one of the indispensable drugs after large blood vessel surgery, effectively preventing patients from postoperative vascular blockage. Professor Wien was awarded the 1982 Nobel Prize in Physiology or Medicine for this important discovery.

Since the advent of aspirin, the medical community has never stopped studying it. So far, aspirin has been found to have more medical uses. In addition to traditional uses, it is also used to prevent digestive system malignancies, breast cancer and melanoma, treat Kawasaki disease (mucocutaneous lymph node syndrome), and can be used as an auxiliary drug for female infertility. In the more than 120 years since aspirin was patented, it has been closely linked to the development of modern medicine and has promoted each other: the birth of aspirin has solved many medical problems, and the progress of medical science has continuously deepened the understanding of the mechanism of action of aspirin.

Reference sources: Popular Science China, "Chemistry", Wandering Pharmaceutical Chemistry, etc.